Pyrrolo[2,1-c][1,4]benzodiazepine antitumour antibiotics are commonly known as anthramycin class of compounds. In the last few years, a growing interest has been shown in the development of new pyrrolo[2,1-c][1,4]benzodiazepines (PBDs). These PBDs are a family of sequence selective DNA-binding antitumour antibiotics that bind exclusively to the exocyclic N2-guanine in the minor groove of DNA via an acid-labile aminal bond to the electophilic imine at the N10-C11 position. (Kunimoto, S.; Masuda, T.; Kanbayashi, N.; Hamada, M.; Naganawa, H.; Miyamoto, M.; Takeuchi, T.; Unezawa, H. J. Antibiot., 1980, 33, 665.; Kohn, K. W.; Speous, C. L. J. Mol. Biol., 1970, 51, 551.; Hurley, L. H. Gairpla, C.; Zmijewski, M. Biochem. Biophys. Acta., 1977, 475, 521.; Kaplan, D. J.; Hurley, L. H. Biochemistry, 1981, 20, 7572.) All biologically active PBDs possess the (S) configuration at the chiral C11a position which provides the molecule with a right-handed twist, which allows them to follow the curvature of the minor groove of B-form double-stranded DNA spanning three base pairs. Recently, PBD dimers have been developed that comprise two C2-exo-methylene-substituted DC-81 subunits tethered through their C-8 position via an inert propanedioxy linker. (Gregson, S. J.; Howard, P. W.; Hartely, J. A.; Brooks N. A.; Adams, L. J.; Jenkins, Kelland, L. R.; Thurston, D. E. J. Med. Chem., 2001, 44, 737.). A recent development has been the linking of two PBD units through their C-8 positions to give bisfunctional alkylating agents capable of cross-linking DNA (Thurston, D. E.; Bose, D. S.; Thomson, A. S.; Howard, P. W.; Leoni, A.; Croker, S. J.; Jenkins, T. C.; Neidle, S.; Hurley, L. H. J. Org. Chem., 1996, 61, 8141–8147). Recently, noncross-linking mixed imine-amide PBD dimers have been synthesized that have significant DNA binding ability and potent anti-tumour activitiy (Kamal A.; Laxman, N.; Ramesh, G.; Ramulu, P.; Srinivas, U.S. Pat. No. 636,233; Kamal, A.; Ramesh, G.; Laxman, N.; Ramulu, P.; Srinivas, O.; Neelima, K.; Kondapi, A. K.; Srinu, V. B.; Nagarajaram, H. M. J. Med. Chem. 2002, 45, 4679.).
PBDs are of considerable current interest due to their ability to recognize and subsequently form covalent bonds to specific base sequences of double-stranded DNA. Naturally occurring pyrrolo[2,1-c][1,4]benzodiazepines belong to a group of antitumour antibiotics derived from Streptomyces species with family members including anthramycin, tomaymycin, sibiromycin, chicamycin, neothramycins A and B, and DC-81.

However, the clinical efficacy for these antibiotics is hindered by several limitations, such as poor water solubility and cardiotoxicity and development of drug resistance and metabolic inactivation.